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BTK-IN-15

CAS No. :

MCE 站：BTK-IN-15

产品活性：BTK-IN-15 是一种新型的布鲁顿酪氨酸激酶 (BTK) 抑制剂，具有良好口服活性。BTK-IN-15 抑制 BTK，IC₅₀ 为 0.7 nM，并具有良好的激酶选择性和抗肿瘤活性，能诱导癌细胞凋亡 (apoptosis)。

研究领域：Protein Tyrosine Kinase/RTK  |  Immunology/Inflammation  |  Apoptosis

作用靶点：Btk  |  Pyroptosis

In Vitro: BTK inhibition is an effective approach against B-cell malignancies.
BTK-IN-15 (compound 42) demonstrates inhibitory against TMD8 with an IC₅₀ value of 2.6 nM.
BTK-IN-15 (1 μM; 1 h) displays significant selectivity to BTK over EGFR kinase with 0.05% ａnd 44% of the control, respectively.
BTK-IN-15 (0-1 mM; 72 h) exerts potent anti-proliferative activity against a human mantle cell lymphoma cell line (REC-1) with an IC₅₀ value of 1.7 nM.
BTK-IN-15 (0-1 mM; 2 h) inhibits BTK auto-phosphorylation with an IC₅₀ value of 1.49 nM.
BTK-IN-15 (0-100 nM; 48 h) arrests cell cycle at G1 phase ａnd (0-1 mM; 72 h) induces apoptosis in TMD8.
BTK-IN-15 shows low hERG channel activity (IC₅₀=4.38 μM), indicating low cardiotoxicity.

In Vivo: BTK-IN-15 (compound 42) (12.5-50 mg/kg; p.o.; twice daily; 21 d) inhibits tumor growth (TGI = 104%) at a dosage of 50 mg/kg in mice.
BTK-IN-15 (300, 400, 500 mg/kg; p.o.; twice daily; 14 d) has biological safety ａnd displays no affect against body weight in mice compared with control.
BTK-IN-15 (10 mg/kg; p.o.) shows a high oral bioavailability of 40.98% in mice.
Pharmacokinetics of BTK-IN-15 in Mice

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